Inhibition of mammalian carbonic anhydrase isoforms I, II and VI with thiamine and thiamine-like molecules
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, cilt.28, sa.2, ss.316-319, 2013 (SCI-Expanded, Scopus)
- Yayın Türü: Makale / Tam Makale
- Cilt numarası: 28 Sayı: 2
- Basım Tarihi: 2013
- Doi Numarası: 10.3109/14756366.2011.637200
- Dergi Adı: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
- Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
- Sayfa Sayıları: ss.316-319
- Anahtar Kelimeler: Carbonic anhydrase, thiamine, inhibition, VITRO INHIBITION, PHENOLIC-COMPOUNDS, ISOZYME-II, SULFONAMIDES, AGENTS, MOIETIES, BINDING, SERIES
- Ondokuz Mayıs Üniversitesi Adresli: Evet
Özet
Here we determined the in vitro inhibitory effects of 5-(2-hydroxyethyl)-3,4-dimethylthiazolium iodide (1), 3-Benzyl-5-(2-hydroxyethyl)-4-methylthiazolium chloride (2) and thiamine (3) on human erythrocyte carbonic anhydrase I, II isozymes (hCA I and hCA II) and secreted isoenzyme CA VI. K I values ranged from 0.38 to 2.27 mu M for hCA I, 0.085 to 0.784 mu M for hCA II and 0.062 to 0.593 mu M for hCA VI, respectively. The compounds displayed relatively strong actions on hCA II, in the same range as the clinically used sulfonamidesethoxzolamide, zonisamide and acetazolamide.